TW200738671A - Compounds for the inhibition of integrins and use thereof - Google Patents

Compounds for the inhibition of integrins and use thereof

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Publication number
TW200738671A
TW200738671A TW096103577A TW96103577A TW200738671A TW 200738671 A TW200738671 A TW 200738671A TW 096103577 A TW096103577 A TW 096103577A TW 96103577 A TW96103577 A TW 96103577A TW 200738671 A TW200738671 A TW 200738671A
Authority
TW
Taiwan
Prior art keywords
substituted
membered rings
group
nrc
radical
Prior art date
Application number
TW096103577A
Other languages
Chinese (zh)
Inventor
Gunther Zischinsky
Roland Stragies
Frank Osterkamp
Dirk Scharn
Gerd Hummel
Holger Kalkhof
Grit Zahn
Doerte Vossmeyer
Claudia Christner-Albrecht
Ulrich Reineke
Original Assignee
Jerini Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Jerini Ag filed Critical Jerini Ag
Publication of TW200738671A publication Critical patent/TW200738671A/en

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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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Abstract

The present invention is related to a compound of formula (I) G-Z-A-Ar-Y-Ψ (I) wherein A is a radical selected from the group comprising nonaromatic heterocyclic and homocyclic ring systems; Ar is a radical which is either absent or present, whereby if Ar is present, Ar is selected from the group comprising 3- to 9-membered rings, or if Ar is present, Ar is a polycyclic ring system selected from the group comprising 4,4-membered rings, 4,5-membered rings, 4,6-membered rings, 5,5-membered rings, 5,6-membered rings, 6,6-membered rings, 6,7-membered rings, 7,7-membered rings, 6,5,6-membered rings, 6,6,6-membered rings, 6,7,6-membered rings; Z and Y are radicals individually and independently selected from the group comprising (CH2)n-E-(CH2)m-L-(CH2)k and (CH2)m-L-(CH2)k, wherein E is a radical which is either absent or present, whereby if E is present, E is selected from the group comprising O, S, NH, NRa, CO, SO, SO2, substituted ethylene and acetylene; L is a radical which is either absent or present, whereby if L is present, L is individually and independently selected from the group comprising O, S, NH, NRb, CO, SO, SO2, substituted ethylene and acetylene; and k, m and n are individually and independently 0, 1, 2 or 3; Ψ is a radical of formula (II), wherein Q is a radical selected from the group comprising a direct bond, C=O, C=S, O, S, CRaRb, NRa-NRb, N=N, CRa=N, N=CRa, (C=O)-O, O-(C=O), SO2, NRa, (C=O)-NRa, NRa-(C=O)-NRb, NRc-(C=O), O-(C=O)-NRc, NRc-(C=O)-O, NRc-(C=S), (C=S)-NRc, NRc-(C=S)-NRd, NRc-SO2 and SO2-NRc. R1, Ra, Rb, Rc and Rd are radicals which are individually and independently selected from the group comprising H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocycloyl, substituted heterocycloyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, cycloalkylalkyl, substituted cycloalkylalkyl, heterocyclylalkyl, substituted heterocyclylalkyl, alkyloxy, alkyloxyalkyl, substituted alkyloxyalkyl, alkyloxycycloalkyl, substituted alkyloxycycloalkyl, alkyloxyheterocyclyl, substituted alkyloxyheterocyclyl, alkyloxyaryl, substituted alkyloxyaryl, alkyloxyheteroaryl, substituted alkyloxyheteroaryl, alkylthioalkyl, substituted alkylthioalkyl, alkylthiocycloalkyl and substituted alkylthiocycloalkyl, hydroxy, substituted hydroxy, oxo, thio, substituted thio, aminocarbonyl, substituted aminocarbonyl, formyl, substituted formyl, thioformyl, substituted thioformyl, amino, substituted amino, hydroxyl, substituted hydroxyl, mercapto, substituted mercapto, hydrazino, substituted hydrazino, diazene, substituted diazene, imine, substituted imine, amidino, substituted amidino, iminomethylamino, substituted iminomethylamino, ureido, substituted ureido, formylamino, substituted formylamino, aminocarbonyloxy, substituted aminocarbonyloxy, hydroxycarbonylamino, substituted hydroxycarbonylamino, hydroxycarbonyl, substituted hydroxycarbonyl, formyloxy, substituted formyloxy, thioformylamino, substituted thioformylamino, ,aminothiocarbonyl, substituted aminothiocarbonyl, thioureido, substituted thioureido, sufonyl, substituted sulfonyl, sulfonamino, substituted sulfonamino, aminosulfonyl, substituted aminosulfonyl, cyano, halogen; R2 is a hydrophobic moiety; R3 is a radical selected from the group comprising OH, C1-C8alkyloxy and aryl C0-C6alkyloxy; R4 is a radical selected from the group comprising hydrogen, halogen and C1-C4alkyl; and G is a radical containing one ore more moieties, whereby such moiety is selected from the group comprising NH, OH and a basic moiety.
TW096103577A 2006-01-31 2007-01-31 Compounds for the inhibition of integrins and use thereof TW200738671A (en)

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EP06002005 2006-01-31

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US (1) US8927534B2 (en)
EP (1) EP1979342A1 (en)
JP (1) JP2009525296A (en)
KR (1) KR20080095854A (en)
CN (1) CN101379056A (en)
AR (1) AR059224A1 (en)
AU (1) AU2007211620A1 (en)
BR (1) BRPI0706800A2 (en)
CA (1) CA2635403A1 (en)
MX (1) MX2008008866A (en)
RU (1) RU2008135358A (en)
TW (1) TW200738671A (en)
WO (1) WO2007088041A1 (en)
ZA (1) ZA200804932B (en)

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